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1
Chakraborty, Santanu, Madhusmruti Khandai, Anuradha Sharma, Ch Patra, V. Patro, and Kalyan Sen. "Effects of drug solubility on the release kinetics of water soluble and insoluble drugs from HPMC based matrix formulations." Acta Pharmaceutica 59, no. 3 (2009): 313–23. http://dx.doi.org/10.2478/v10007-009-0025-8.
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Effects of drug solubility on the release kinetics of water soluble and insoluble drugs from HPMC based matrix formulations The purpose of the present research work was to observe the effects of drug solubility on their release kinetics of water soluble verpamil hydrochloride and insoluble aceclofenac from hydrophilic polymer based matrix formulations. Matrix formulations were prepared by the direct compression method. The formulations were evaluated for various physical parameters. Along with the dynamics of water uptake and erosion, SEM and in vitro drug release of the tablets were studied. Applying an exponential equation, it was found that the kinetics of soluble drug release followed anomalous non-Fickian diffusion transport whereas insoluble drug showed zero-order release. SEM study showed pore formation on the tablet surface that differed depending on drug solubility. t-Test pointed to a significant difference in amount of both drugs released due to the difference in solubility. Solubility of the drug effects kinetics and the mechanism of drug release.
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Nooreen, Hari kiriti varma G, and Vijayakuchana. "Formulation and in vitro evaluation of sustained release matrix tablets of Rimopride Citrate Dihydrate." Frontier Journal of Pharmaceutical Sciences and Research 7, no. 1 (2024): 1–5. https://doi.org/10.5281/zenodo.10575985.
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Drugs are most frequently administered by oral route. Although a few drugs taken orally are intended to be dissolved in the mouth, nearly all drugs taken orally are swallowed. A few drugs such as antacids are swallowed for their local action in the gastrointestinal tracts. Hence the above study demonstrated that combination of HPMC K4M and HPMC K15M can be used to formulate sustained release matrix tablets of Rimopride Citrate Dihydrate. This can sustain the drug release up to 24 hours as per standard dissolution profile. This can be expected to reduce the frequency of administration and decrease the dose – dependent side effects associated with repeated administration of conventional Rimopride Citrate Dihydrate dihydrate tablets. The cumulative drug release of innovators brand (MOZA SR, Intas Pharmaceuticals) of sustained release tablet of Rimopride Citrate Dihydrate were compared for in vitro dissolution study. The formulation F9 matrix tablet releases the drug appropriately in comparison of innovators brand. The cumulative drug release at the end of 24th hour from formulation F9 (98.01%) and the cumulative drug release at the end of 24th hour from innovators brand was (97.30%). The in vitro drug release result indicates that formulation F9 released more drug than innovators brand and hence more drug is available at the absorption site from formulation F9 as compared to innovators brand, hence the formulation F9 has better bioavailability than innovators brand of Rimopride Citrate Dihydrate sustained release matrix tablet and also the sustained release matrix tablet was found to be beneficial in terms of reduction in frequency of administration. The formulation F9 best suited with zero order release kinetics (corr.coefficient =0.943) than the first order release kinetics (corr. Coefficient = 0.910). The formulation F9 follows Higuchi model of drug release kinetics (corr. coefficient=0.41). The Koresmyer peppas drug release kinetics showed correlation coefficient (0.926) and release exponent (n) 0.724 which indicates that the drug release mechanism is non-fickanian diffusion. Hence it can be concluded that once daily sustain release matrix tablet of Rimopride Citrate Dihydrate having short half life, was found to exert a satisfactory sustained release profile which may provide an improved bioavailability, increased therapeutic efficacy and patient compliance.
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Kumar, Putta Rajesh, Meena N, Poojitha P, Sowjanya P, Shivaleela U, and Sharma JVC. "Formulation Design and in Vitro Evaluation Studies of Antidepressant Venlafaxine Hydrochloride Oral Drug Delivery Systems." Journal of Biomedical and Pharmaceutical Research 13, no. 2 (2024): 51–63. http://dx.doi.org/10.32553/jbpr.v13i2.1084.
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Background: Venlafaxine Hydrochloride a serotonin, nor epinephrine reuptake inhibitor, oral antidepressant used to treat depression. Objective: The present study was aimed at studying controlled release of Venlafaxine Hydrochloride with Guargum, Hydroxy propyl methyl cellulose as matrix polymers, Micro crystalline cellulose as binder and Dicalcium phosphate as diluent filler. Methods: Tablets were studied for pre, post compression, swelling and in vitro dissolution studies. Drug release was analyzed by release kinetic models. Results: Preformulation studies revealed that the drug procured was pure. Analytical method was linear and precise. The rheological parameters were within the ideal limits and suitable for compression. Swelling index increased with increase in matrix polymer content. In vitro studies showed drug release, sustained for 18 to 24 h. Optimized formulation V5 released 14.32±0.430% in 2 h. At the end of 12 and 24 h it has released 49.37±0.685% and 98.31±0.435% of drug respectively and followed peppa’s kinetics with anomalous (Non fickian) diffusion mechanism of drug release. Discussion: The drug release from swollen gel matrix occurred initially by drug diffusion followed by polymer chain relaxation and erosion. The in vitro release kinetics from majority of formulations followed Peppa’s and zero order kinetics. The peppa’s n values indicated drug release via anomalous (non fickian) diffusion and super case II transport. Conclusion: Venlafaxine HCl release form tablets sustained up to 24 h which could provide better bioavailability and improved patient compliance. Keywords: Venlafaxine HCl, controlled release matrix tablets, guar gum, Hydroxy propyl methyl cellulose, In vitro studies, Release kinetics.
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Zhu, Weiwei, Jiajie Long, and Meiwu Shi. "Release Kinetics Model Fitting of Drugs with Different Structures from Viscose Fabric." Materials 16, no. 8 (2023): 3282. http://dx.doi.org/10.3390/ma16083282.
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(1) Background: It is simpler and more environmentally friendly to use supercritical CO2 fluid technology to process skincare viscose fabrics. Therefore, it is significant to study the release properties of drug-loaded viscose fabrics to choose suitable skincare drugs. In this work, the release kinetics model fittings were investigated in order to clarify the release mechanism and provide a theoretical basis for processing skincare viscose fabrics with supercritical CO2 fluid. (2) Methods: Nine kinds of drugs with different substituent groups, different molecular weights, and different substitution positions were loaded onto viscose fabrics using supercritical CO2 fluid. Then, the drug-loaded viscose fabrics were placed in an ethanol medium, and the release curves were drawn. Finally, the release kinetics were fitted using zero-order release kinetics, the first-order kinetics model, the Higuchi model, and the Korsmeyer–Peppas model. (3) Results: The Korsmeyer–Peppas model was the best-fitting model for all the drugs. Drugs with different substituent groups were released via a non-Fickian diffusion mechanism. On the contrary, other drugs were released via a Fickian diffusion mechanism. (4) Conclusions: In view of the release kinetics, it was found that the viscose fabric can swell when a drug with a higher solubility parameter is loaded onto it using supercritical CO2 fluid, and the release rate is also slower.
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Arefin, Paroma, Ikramul Hasan, Md Shfiqul Islam, and Md Selim Reza. "Formulation and In vitro Evaluation of Eudragit RL 100 Loaded Fexofenadine HCl Microspheres." Bangladesh Pharmaceutical Journal 19, no. 1 (2016): 58–67. http://dx.doi.org/10.3329/bpj.v19i1.29240.
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The present study deals with the formulation and evaluation of Fexofenadine hydrochloride (HCl) loaded sustained release microspheres by emulsion solvent evaporation method with Eudragit RL 100. The effects of percent drug loading on drug encapsulation efficiency, drug content and drug release rate were assessed. In vitro dissolution study was performed spectrophotometrically according to USP paddle method using phosphate buffer (pH 6.8) for 10 hours. The release rate of Fexofenadine HCl from the microspheres was significantly increased with the increase of drug loading. The drug release patterns were simulated in different kinetic orders such as zero order release kinetics, first order release kinetics, Higuchi release kinetics, Korsmeyer-Peppas release kinetics and Hixson-Crowell release kinetics to assess the release mechanism and Higuchi release kinetics was found to be the predominant release mechanism. Morphological changes due to different drug loading were assessed by scanning electron microscopic (SEM) technique. Differential scanning calorimetry and fourier transform infra-red (FT-IR) spectroscopy was performed to evaluate compatibility of drug with the polymer. A statistically significant variation indrug encapsulation efficiency and release rate was observed for variation in drug loading.Bangladesh Pharmaceutical Journal 19(1): 58-67, 2016
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Mitran, Raul-Augustin, Daniela Berger, Jeanina Pandele-Cusu, and Cristian Matei. "Effect of Aluminum Incorporation into Mesoporous Aluminosilicate Framework on Drug Release Kinetics." Journal of Nanomaterials 2017 (2017): 1–9. http://dx.doi.org/10.1155/2017/9864396.
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Mesoporous silica materials are promising nanocarriers for the development of drug delivery systems. In this study, the influence of pore size, volume, surface area, and doping the silica framework on the release kinetics of a model drug, metoprolol, has been studied. 20% or 50% wt. therapeutic agent was loaded into the carrier mesopores through incipient wetness impregnation. The carriers and drug-loaded samples have been characterized by small- and wide-angle X-ray diffraction, FT-IR spectroscopy, scanning electron microscopy, and nitrogen adsorption-desorption isotherms. The in vitro release profiles have been fitted using a three-parameter kinetic model and they have been explained in terms of the release rate during the burst and sustained release stages and the fraction of drug molecules released during the burst stage. The silica framework doping with aluminum was found to decrease the amount of drug released in the burst stage, without affecting the other kinetic parameters. The therapeutic agent release rates depend mainly on the pore size and volume of the mesoporous carriers and drug-loaded samples.
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Suprianto. "Analisis Kinetika Pelepasan Teofilin dari Granul Matriks Kitosan." JURNAL ILMIAH MANUNTUNG 2, no. 1 (2016): 70–80. https://doi.org/10.5281/zenodo.1246129.
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Moment the drug dosage form development, it is important to study the drug release or dissolution that is recognized as an element in drug development. Mathematical models could help optimize the design of drugs to produce models of drug release information. Analysis of quantitative values obtained when depicting dissolution drug release profiles more easily when the mathematical concepts used to describe the drug release kinetics model. The model release of drugs known includes zero order, first order, Higuchi models, models Hixon Crowell and Peppas Korsmeyer models. The purpose of this review applies mathematical concepts to study the phenomenon of the drug release theophylline granules matrix made from chitosan.
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Dumitriu, Raluca Petronela, Ana Maria Oprea, and Cornelia Vasile. "Kinetics of Swelling and Drug Release from PNIPAAm/Alginate Stimuli Responsive Hydrogels." Solid State Phenomena 154 (April 2009): 17–22. http://dx.doi.org/10.4028/www.scientific.net/ssp.154.17.
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Stimuli responsive hydrogels are very attractive for applications in sustained and/or targeted drug delivery systems. As the release of drugs is related to the swelling behavior of hydrogels, the swelling kinetic studies become of great importance to appreciate the release kinetics from hydrogel matrices. Hydrogels with high performance properties have been prepared from N-isopropylacryl amide (NIPAAm) and sodium alginate, crosslinked with N,N`-methylene-bis-(acrylamide) (MBAAm). This study is focused on the investigation of swelling and drug release kinetics, coupled by morphological studies. The kinetic parameters of the swelling at different temperatures for hydrogels samples have been evaluated and confirmed their temperature-responsive behavior. The swelling rate constant (ksw) decreases of with increasing temperature and slight increases with the alginate content in the samples. The drug release kinetic study from the prepared hydrogel matrices was performed in twice-distilled water and ethanol for bioactive agents as vanillin and ketoprofen, respectively. An increase of alginate content results in a slower rate and smaller percentage of vanillin and ketoprofen released. It has been established that the ketoprofen occurs according with case II of transport and vanillin release behavior occurs by an anomalous transport mechanism. The values of the release rate constant (kr) decreased by increasing swelling degree in case of 75/25 NIPAAm/alginate hydrogels and decreased also by increasing content of alginate in hydrogels with various compositions. Morphological studies performed by environmental scanning electron microscopy (ESEM) evidenced a relaxed network at high relative humidity, which explain both swelling and release profiles.
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Das, Utpal, Shimul Halder, Abul Kalam Lutful Kabir, Harun Or Rashid, and Abu Shara Shamsur Rouf. "Development and in vitro Evaluation of Sustained Release Matrix Tablets of Indapamide from Methocel® K15 MCR and K100 LVCR." Dhaka University Journal of Pharmaceutical Sciences 10, no. 2 (2012): 87–92. http://dx.doi.org/10.3329/dujps.v10i2.11785.
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Indapamide, a low-dose thiazide-type diuretic, is used for the treatment of essential hypertension. In this study, we developed an indapamide sustained release formulation using Methocel K15 MCR (a modified hydroxypropyl methylcellulose), Methocel K100 LVCR (a modified hydroxypropyl methylcellulose), magnesium stearate, talc and starch 1500 by direct compression. The powders for tableting were evaluated for angle of repose, loose bulk density, tapped bulk density, compressibility index, total porosity etc. The tablets were subjected to thickness, weight variation test, hardness, friability and in vitro release studies. The in vitro dissolution study was carried out in the gastric medium (pH 1.3) for first two hours and then in the intestinal medium (pH 6.8) for 22 hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus. The granules showed satisfactory flow properties, compressibility index etc. All the tablets complied with pharmacopoeial specifications. The results of dissolution studies indicated that the formulation F-5 and F-7 (up to 75.36 % drug release in 12 hours) could extend the drug release up to 12 hours. The drug release patterns were simulated in different kinetic orders such as Zero Order release kinetics, First Order release kinetics, Higuchi release kinetics, Korsmeyer-Peppas release kinetics and Hixson-Crowell release kinetics to assess the release mechanism. From the study we observed that Higuchi release kinetics was the predominant release mechanism than Zero Order and First Order kinetics. The drug release mechanism from the matrix tablets was found to be non Fickian mechanism. DOI: http://dx.doi.org/10.3329/dujps.v10i2.11785 Dhaka Univ. J. Pharm. Sci. 10(2): 87-92, 2011 (December)
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Loew, Stephan, Alfred Fahr, and Sylvio May. "Modeling the Release Kinetics of Poorly Water-Soluble Drug Molecules from Liposomal Nanocarriers." Journal of Drug Delivery 2011 (June 7, 2011): 1–10. http://dx.doi.org/10.1155/2011/376548.
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Liposomes are frequently used as pharmaceutical nanocarriers to deliver poorly water-soluble drugs such as temoporfin, cyclosporine A, amphotericin B, and paclitaxel to their target site. Optimal drug delivery depends on understanding the release kinetics of the drug molecules from the host liposomes during the journey to the target site and at the target site. Transfer of drugs in model systems consisting of donor liposomes and acceptor liposomes is known from experimental work to typically exhibit a first-order kinetics with a simple exponential behavior. In some cases, a fast component in the initial transfer is present, in other cases the transfer is sigmoidal. We present and analyze a theoretical model for the transfer that accounts for two physical mechanisms, collisions between liposomes and diffusion of the drug molecules through the aqueous phase. Starting with the detailed distribution of drug molecules among the individual liposomes, we specify the conditions that lead to an apparent first-order kinetic behavior. We also discuss possible implications on the transfer kinetics of (1) high drug loading of donor liposomes, (2) attractive interactions between drug molecules within the liposomes, and (3) slow transfer of drugs between the inner and outer leaflets of the liposomes.
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Debatri, Roy, Das Sudipta, Panda Anumoy, et al. "Development and Comparative Analysis of Metronidazole Microspheres Prepared with Different Combinations of Polymers Using Ionotropic Gelation Technique." Indian Journal of Science and Technology 16, no. 42 (2023): 3821–28. https://doi.org/10.17485/IJST/v16i42.2293.
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Abstract <strong>Objective:</strong> Basis of this experiment was progressive preparation and evaluation of generated metronidazole loaded microsphere by desired ratio of polymers which can improve its therapeutic efficacy and reduce the need for frequent dosing. The use of microspheres can improve the bioavailability of the medication by protecting it from degradation and improving its absorption in the body. Drug release pattern can be altered by swelling Index and diffusion.<strong> Methods:</strong> Metronidazole loaded microsphere was prepared by ionotropic gelation technique using different combination of polymers, such as of Sodium alginate, Hydroxy propyl methylcellulose and Carbopol. Evaluation process for microspheres was performed by size analysis, percentage yield, swelling index, drug entrapment efficiency, drug release study (In-Vitro), kinetics models (Zero order, First order, Higuchi, Hixon-Crowell and Korsmeyers- Peppas) and stability testing. <strong>Findings:</strong> The average sizes of F1, F2 and F3 were observed and F2 had the lowest particle size. Swelling index was observed for all formulations, and F3 had the highest swelling property about 90%. During in-vitro drug release study it was noticed that F2 gives the highest percentage of drug release about 88.44% in comparison to other batches. Drug release kinetic study shows that F2 follows zero order and Higuchi model mostly with R2 value 0.9987 and 0.9861 respectively. Stability study report for F2 batch was also acceptable for this study. <strong>Novelty:</strong> Previous researches was concentrated on controlled drug release study, bioavailability improvements and for dosage frequency reduction. But novelty of this project is to improve swelling potentiality of formulations by Ionotropic gelation techniques and finding out the association in between swelling property, drug diffusion and release kinetics of drugs that was not detected in prior studies. Also, this study determines better combination of hydrophilic polymer with respect to drug release property and improved release kinetics. <strong>Keywords:</strong> Metronidazole, Ionotropic gelation technique, Sodium alginate, Hydroxypropyl methylcellulose, Carbopol, drug release kinetics
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Gierszewska, Magdalena, Jadwiga Ostrowska-Czubenko, and Ewelina Chrzanowska. "CHARACTERISTICS OF ASCORBIC ACID RELEASE FROM TPP-CROSSLINKED CHITOSAN/ALGINATE POLYELECTROLYTE COMPLEX MEMBRANES." Progress on Chemistry and Application of Chitin and its Derivatives XXIII (September 10, 2018): 76–87. http://dx.doi.org/10.15259/pcacd.23.007.
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Chitosan/alginate polyelectrolyte complex membranes (Ch/Alg) additionally cross-linked with tripolyphosphate (TPP) and containing ascorbic acid (AA) were prepared. The dynamic swelling behaviour of Ch/Alg/TPP and ascorbic acid release from the membrane were characterised in different buffer solutions. It has been found that the pH of the buffer solution affects the swelling and release behaviour of AA. Ascorbic acid release, observed over a period of 360 min, exhibited a biphasic pattern, characterised by a fast initial burst release, followed by a slow, sustained release. Different mathematical models were used to study the kinetics and transport mechanism of AA from Ch/Alg/TPP hydrogels. Drug release data were fitted to the zero order kinetic model and first order kinetic model. To characterise the drug mechanism, the release data were fitted to the Higuchi and Korsmeyer-Peppas equations. The initial burst AA release followed zero order kinetics and was quasi-Fickian in nature. The second step of AA release followed first order kinetics.
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Chudoba, Dorota, Monika Jażdżewska, Katarzyna Łudzik, Sebastian Wołoszczuk, Ewa Juszyńska-Gałązka, and Mikołaj Kościński. "Description of Release Process of Doxorubicin from Modified Carbon Nanotubes." International Journal of Molecular Sciences 22, no. 21 (2021): 12003. http://dx.doi.org/10.3390/ijms222112003.
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The article discusses the release process of doxorubicin hydrochloride (DOX) from multi-wall carbon nanotubes (MWCNTs). The studies described a probable mechanism of release and actions between the surface of functionalized MWCNTs and anticancer drugs. The surface of carbon nanotubes (CNTs) has been modified via treatment in nitric acid to optimize the adsorption and release process. The modification efficiency and physicochemical properties of the MWCNTs+DOX system were analyzed by using SEM, TEM, EDS, FTIR, Raman Spectroscopy and UV-Vis methods. Based on computer simulations at pH 7.4 and the experiment at pH 5.4, the kinetics and the mechanism of DOX release from MWNT were discussed. It has been experimentally observed that the acidic pH (5.4) is appropriate for the efficient release of the drug from CNTs. It was noted that under acidic pH conditions, which is typical for the tumour microenvironment almost 90% of the drug was released in a relatively short time. The kinetics models based on different mathematical functions were used to describe the release mechanism of drugs from MWCNTs. Our studies indicated that the best fit of experimental kinetic curves of release has been observed for the Power-law model and the fitted parameters suggest that the drug release mechanism of DOX from MWCNTs is controlled by Fickian diffusion. Molecular dynamics simulations, on the other hand, have shown that in a neutral pH solution, which is close to the blood pH, the release process does not occur keeping the aggregation level constant. The presented studies have shown that MWCNTs are promising carriers of anticancer drugs that, depending on the surface modification, can exhibit different adsorption mechanisms and release.
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Nining, Nining, Anisa Amalia, and Raditya Naufal Riyanto. "The effect of HPMC-K15M and guar gum as polymer-coated for sustained-released tablet: disintegration and release kinetics." Pharmaciana 14, no. 3 (2024): 396–407. https://doi.org/10.12928/pharmaciana.v14i3.28104.
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Polymeric coating films are able to control tablet drug release rate depending on polymer physicochemical properties. Guar gum and HPMC-K15M (GG/HPMC-K15M) can be a coating polymer in sustained-release tablets. This study aims to characterize the disintegration and drug release kinetics on theophylline sustained-release tablets coated with GG/HPMC-K15M. The film coating was made with variations of the GG/HPMC-K15M ratio of 1:3 (F1), 1:4 (F2), and 1:5 (F3). Granules were preformulated regarding LOD, granule size distribution, packing, and flow properties. Film coating was carried out using a liquid spraying method. Coated tablets were tested for quality examination, and the drug release kinetics model was determined based on in-vitro dissolution. Granule pre-formulation result shows that the granules have excellent packing and flow properties with an LOD of 4.59–5.33% and a size of 553.28–627.28 πm. Tablets provided uniform size characteristics with a weight variation of 333.38–339.56 mg (CV 1.32–3.43% and acceptance value 6.53–13.58), hardness of 11.61–18.86 kgf, friability of 0.103–0.186%, disintegration time of 20.69–27.36 min, and drug content of 98.51–98.55%. The theophylline was dissolved by 95.24% (6h in FI), 97.04% (7h in F2), and 99.79% (8h in F3); all formulas followed zero-order kinetic (r2 ~ 1). Suitable quality theophylline tablets GG/HPMC-K15M coating have been successfully produced. Increasing the concentration ratio of HPMC-K15M in the coating solution resulted in a significant increase in disintegration time and a slowing of the drug release rate. The drug release kinetics of all formulations followed the zero-order kinetic model.
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Wani, Taha Umair, and Nisar Ahmad Khan. "Formulation of Carbopol Capsules for Sustained Release of Losartan Potassium." Journal of Drug Delivery and Therapeutics 9, no. 2-s (2019): 92–97. http://dx.doi.org/10.22270/jddt.v9i2-s.2468.
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Sustained release formulations have been extensively studied for their benefits in improving various physicochemical and pharmacokinetic properties of large number of drugs. The aim of this study was to develop and evaluate sustained release capsules of losartan potassium in order to provide drug release over a long period of time. This allows the drug much time for absorption in gastrointestinal tract (GIT) and hence may increase the bioavailability of the drug. Carbopol 971 P was used as rate controlling polymer for the preparation of capsules. The capsules were evaluated for matrix integrity and drug release using USP type II dissolution apparatus. The sustained release capsules showed excellent matrix integrity and released more than 90% of the drug over a period of 12 hours. The kinetic studies showed that the drug release from the carbopol matrices followed Korsmeyer Peppas release kinetics and hence the mechanism of drug release was a combination of more than one processes i.e. diffusion and erossion. Hydration volume as well as matrix integrity were affected by the change in the amount of the polymer in the capsules. The study suggests that carbopol 971P capsules can be efficiently used to control and extend the release of losartan potassium over a long period. Thus improved absorption and bioavailability can be achieved which requires further studies in animals in future. Keywords: Sustained release, Carbopol, Hydration volume, Capsules
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Kusum, ,., Avinash Kumar Gupta, Manish Kumar Gupta, and Vijay Sharma. "A Review on Formulation and Evaluation of Sustained Release Tablet of Devilproex Sodium." Journal of Drug Delivery and Therapeutics 9, no. 4 (2019): 660–62. http://dx.doi.org/10.22270/jddt.v9i4.3067.
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An appropriately designed drug delivery system can be a major step towards solving these two problems. This technique for the drug administration is termed as ‘sustained release’ or ‘controlled release. Drugs with dosage not exceeding 125mg – 325mg are more suited as extended release products in order to limit the size of the delivery system. In the case of soluble matrix the matrix swells or dissolves. These matrices then undergo surface erosion with little or no bulk erosion. Divalproex sodium dissociates to the valproate ion in the gastrointestinal tract. The mechanisms by which valproate exerts its therapeutic effects have not been established. One of its most important characteristics is the high gelation velocity and viscosity, which has a significant effect on the release kinetics of the incorporated drug. It was proven that HPMC at high concentration promoted the drug release approaching to a zero-order release kinetic because of its gelation properties Keywords: HPMC, Divalproex sodium, sustained release and zero-order release kinetic
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Ekenna, Ifeoma Cynthia, and Sunday Okorie Abali. "Comparison of the Use of Kinetic Model Plots and DD Solver Software to Evaluate the Drug Release from Griseofulvin Tablets." Journal of Drug Delivery and Therapeutics 12, no. 2-S (2022): 5–13. http://dx.doi.org/10.22270/jddt.v12i2-s.5402.
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Awareness of the release kinetics of active drugs is important in formulating drugs that have the desired delivery and in predicting the behaviour of the formulated drug in vivo. The study aims to determine the mechanism of drug release from griseofulvin tablets formulated with different surfactants using mathematical models and to compare the use of graphs and DD solver software in fitting dissolution profiles to kinetic models. The batches P1 -P3 were composed of the surfactant - PEG 4000 in different concentrations. A control batch without surfactant and a commercial brand (Mycoxyl 500) were used for comparison. Granule and tablet quality tests indicated quality formulations. Dissolution profiles showed that the surfactant improved drug release of griseofulvin and batches (batches P1 -P3) formulated with PEG 4000 had the best release profiles comparable with the commercial brand. The Excel Add-in DD solver and kinetic plots were used to determine the kinetic model of best fit. The Higuchi model was the best fit for batches P1 -P3. The first order and Hixon -Crowell also fit batches P2 and P3. The Korsmeyer’s model showed that batches P1 -P3 exhibited anomalous diffusion. The tablets formulated with PEG were as good as the commercial brand and they had an anomalous diffusion of the drug from the tablet; meaning that drug diffused following Fickian law and also diffused through a swollen and porous matrix. Kinetic plots and the DD solver can be used for fitting dissolution profiles to kinetic models.
 Keywords: Griseofulvin, Kinetics, Models, Surfactants, Polyethylene glycol (PEG) 4000, DD solver, Dissolution profile, mathematical models
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Ekenna, Ifeoma Cynthia, and Sunday Okorie Abali. "Comparison of the Use of Kinetic Model Plots and DD Solver Software to Evaluate the Drug Release from Griseofulvin Tablets." Journal of Drug Delivery and Therapeutics 12, no. 2-S (2022): 5–13. http://dx.doi.org/10.22270/jddt.v12i2-s.5402.
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Awareness of the release kinetics of active drugs is important in formulating drugs that have the desired delivery and in predicting the behaviour of the formulated drug in vivo. The study aims to determine the mechanism of drug release from griseofulvin tablets formulated with different surfactants using mathematical models and to compare the use of graphs and DD solver software in fitting dissolution profiles to kinetic models. The batches P1 -P3 were composed of the surfactant - PEG 4000 in different concentrations. A control batch without surfactant and a commercial brand (Mycoxyl 500) were used for comparison. Granule and tablet quality tests indicated quality formulations. Dissolution profiles showed that the surfactant improved drug release of griseofulvin and batches (batches P1 -P3) formulated with PEG 4000 had the best release profiles comparable with the commercial brand. The Excel Add-in DD solver and kinetic plots were used to determine the kinetic model of best fit. The Higuchi model was the best fit for batches P1 -P3. The first order and Hixon -Crowell also fit batches P2 and P3. The Korsmeyer’s model showed that batches P1 -P3 exhibited anomalous diffusion. The tablets formulated with PEG were as good as the commercial brand and they had an anomalous diffusion of the drug from the tablet; meaning that drug diffused following Fickian law and also diffused through a swollen and porous matrix. Kinetic plots and the DD solver can be used for fitting dissolution profiles to kinetic models.
 Keywords: Griseofulvin, Kinetics, Models, Surfactants, Polyethylene glycol (PEG) 4000, DD solver, Dissolution profile, mathematical models
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Sha’at, Mousa, Lacramioara Ochiuz, Cristina Marcela Rusu, et al. "Experimental and Theoretical Design on the Development of Matrix Tablets with Multiple Drug Loadings Aimed at Optimizing Antidiabetic Medication." Pharmaceutics 16, no. 12 (2024): 1595. https://doi.org/10.3390/pharmaceutics16121595.
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Background: Diabetes is a growing global health crisis that requires effective therapeutic strategies to optimize treatment outcomes. This study aims to address this challenge by developing and characterizing extended-release polymeric matrix tablets containing metformin hydrochloride (M-HCl), a first-line treatment for type 2 diabetes, and honokiol (HNK), a bioactive compound with potential therapeutic benefits. The objective is to enhance glycemic control and overall therapeutic outcomes through an innovative dual-drug delivery system. Methods: The tablets were formulated using hydrophilic polymers, such as Carbopol® 71G NF and Noveon® AA-1. The release kinetics of M-HCl and HNK were investigated through advanced mathematical models, including fractal and multifractal dynamics, to capture the non-linear and time-dependent release processes. Traditional kinetic models (zero-order, first-order, Higuchi equations) were also evaluated for comparison. In vitro dissolution studies were conducted to determine the release profiles of the active ingredients under varying polymer concentrations. Results: The study revealed distinct release profiles for the two active ingredients. M-HCl exhibited a rapid release phase, with 80% of the drug released within 4–7 h depending on polymer concentration. In contrast, HNK demonstrated a slower release profile, achieving 80% release after 9–10 h, indicating a greater sensitivity to polymer concentration. At shorter intervals, drug release followed classical kinetic models, while multifractal dynamics dominated at longer intervals. Higher polymer concentrations resulted in slower drug release rates due to the formation of a gel-like structure upon hydration, which hindered drug diffusion. The mechanical properties and stability of the matrix tablets confirmed their suitability for extended-release applications. Mathematical modeling validated the experimental findings and provided insights into the structural and time-dependent factors influencing drug release. Conclusions: This study successfully developed dual-drug extended-release matrix tablets containing metformin hydrochloride and honokiol, highlighting the potential of hydrophilic polymers to regulate drug release. The findings emphasize the utility of advanced mathematical models for predicting release kinetics and underscore the potential of these formulations to improve patient compliance and therapeutic outcomes in diabetes management.
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Sreekanth Reddy, O., M. C. S. Subha, T. Jithendra, C. Madhavi, and K. Chowdoji Rao. "Fabrication of Gelatin/Karaya gum blend microspheres for the controlled release of Distigmine bromide." Journal of Drug Delivery and Therapeutics 9, no. 3-s (2019): 1–11. http://dx.doi.org/10.22270/jddt.v9i3-s.2720.
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This paper reports the fabrication of gelatin/karaya gum microspheres by emulsion crosslinking method for controlled release of distigmine bromide. The microspheres were crosslinked with the help of glutaraldehyde and used for controlled oral delivery of distigmine bromide. The obtained microspheres were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction and scanning electron microscopy. Drug release kinetics of the microspheres is investigated in simulated intestinal fluid pH 7.4 at 37oC. Results illustrated that microspheres was influenced by the pH of test mediums, which might be suitable for intestinal drug delivery. The drug release kinetics was analyzed by evaluating the release data using different kinetic models. Keywords: Karaya Gum, Gelatin, microspheres, drug delivery.
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Saini, Mohit. "Release Kinetic Study of Matrix Type Transdermal Patch Using anAnalgesic Drug." IAR Journal of Medicine and Surgery Research 1, no. 1 (2020): 1–8. http://dx.doi.org/10.70818/iarjmsr.2020.v01i01.01.
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Transdermal therapeutic systems are defined as a self-contained, distinct dosage forms which, when applied to the intact skin, deliver the drug, through the skin at control rate to the systemic circulation. TDDS characterizes one of the most quickly advancing areas of novel drug delivery. TDDS are designed for controlled liberate of drug through the skin into systemic circulation maintaining consistent efficacy and reducing dose of the drug and its related side effects. Present study was conducted to prepare transdermal patch of Tramadol HCL with permeation enhancer to diminish extra side effects and to provide sustain drug delivery. Various kinetics models were examined for optimized formulation. The drug release data of all the formulation were fitted to different kinetic models to find out the kinetics of drug release from transdermal patch. The drug release data was also fitted to zero order (cumulative amount of drug release vs. time) power equation to find out the drug release mechanism.
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Khan, Kamran Ahmad, Gul Majid Khan, Muhammad Muzammal, et al. "Preparation of Losartan Potassium Controlled Release Matrices and In-Vitro Investigation Using Rate Controlling Agents." Molecules 27, no. 3 (2022): 864. http://dx.doi.org/10.3390/molecules27030864.
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Controlled release matrices have predictable drug release kinetics, provide drugs for an extended period of time, and reduce dosing frequency with improved patient compliance as compared with conventional tablet dosage forms. In the current research work, losartan potassium controlled release matrix tablets were fabricated and prepared with rate altering agents; that is, Ethocel grade 100 combined with Carbopol 934PNF. Various drug to polymer ratios were used. HPMC, CMC, and starch were incorporated in some of the matrices by replacing some amount of filler (5%). The direct compression method was adopted for the preparation of matrices. In phosphate buffer (pH 6.8), the dissolution study was conducted by adopting the USP method-I as the specified method. Drug release kinetics was determined and dissolution profiles were also compared with the reference standard. Prolonged release was observed for all matrices, but those with Ethocel 100FP Premium showed more extended release. The co-excipient (HPMC, CMC, and starch) exhibited enhancement in the drug release rates, while all controlled release matrices released the drug by anamolous non-Fickian diffusion mechanism. This combination of polymers (Ethocel grade 100 with Carbopol 934PNF) efficiently extended the drug release rates up to 24 h. It is suggested that these matrix tablets can be given in once a day dosage, which might improve patient compliance, and the polymeric blend of Ethocel grade 100 with Carbopol 934PNF might be used in the development of prolonged release matrices of other water-soluble drugs.
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Yang, Keni, Karolina Tran, and Anna Salvati. "Tuning Liposome Stability in Biological Environments and Intracellular Drug Release Kinetics." Biomolecules 13, no. 1 (2022): 59. http://dx.doi.org/10.3390/biom13010059.
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Ideal drug carriers should be stable in biological environments but eventually release their drug load once inside the targeted cells. These two aspects can be in contrast with each other, thus they need to be carefully tuned in order to achieve the desired properties for specific applications. Quantifying drug release profiles in biological environments or inside cells can be highly challenging, and standard methods to determine drug release kinetics in many cases cannot be applied to complex biological environments or cells. Within this context, the present work combined kinetic studies by flow cytometry with aging experiments in biological fluids and size-exclusion chromatography to determine drug release profiles in biological environments and inside cells. To this purpose, anionic and zwitterionic liposomes were used as model nanomedicines. By changing lipid composition, liposome stability in serum and intracellular release kinetics could be tuned and formulations with very different properties could be obtained. The methods presented can be used to characterize liposome release profiles in complex biological media, as well as inside cells. In this way, liposome composition can be tuned in order to achieve formulations with optimal balance between stability and release kinetics for specific applications.
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Quesada-Pérez, Manuel, Luis Pérez-Mas, David Carrizo-Tejero, José-Alberto Maroto-Centeno, María del Mar Ramos-Tejada, and Alberto Martín-Molina. "Coarse-Grained Simulations of Release of Drugs Housed in Flexible Nanogels: New Insights into Kinetic Parameters." Polymers 14, no. 21 (2022): 4760. http://dx.doi.org/10.3390/polym14214760.
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The diffusion-controlled release of drugs housed in flexible nanogels has been simulated with the help of a coarse-grained model that explicitly considers polymer chains. In these in silico experiments, the effect of its flexibility is assessed by comparing it with data obtained for a rigid nanogel with the same volume fraction and topology. Our results show that the initial distribution of the drug can exert a great influence on the release kinetics. This work also reveals that certain surface phenomena driven by steric interactions can lead to apparently counterintuitive behaviors. Such phenomena are not usually included in many theoretical treatments used for the analysis of experimental release kinetics. Therefore, one should be very careful in drawing conclusions from these formalisms. In fact, our results suggest that the interpretation of drug release curves in terms of kinetic exponents (obtained from the Ritger–Peppas Equation) is a tricky question. However, such curves can provide a first estimate of the drug diffusion coefficient.
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Batul, Rahila, Abdul Khaliq, Ahmed Alafnan, Mrinal Bhave, and Aimin Yu. "Investigation of Gentamicin Release from Polydopamine Nanoparticles." Applied Sciences 12, no. 13 (2022): 6319. http://dx.doi.org/10.3390/app12136319.
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Polydopamine (PDA), being highly reactive in nature, has acquired great attention in multi-disciplinary fields. Owing to its fascinating properties, including its biocompatible, non-toxic and readily bio-degradative nature, we investigated the drug loading and release behavior, using an aminoglycoside antibiotic gentamicin (G) as a model drug. The gentamicin was loaded into the PDA nanoparticles (NPs) via an in situ polymerization method. The release kinetics of the gentamicin was then studied in pH 3, 5 and 7.4. Two batches with varied gentamicin loadings, G-PDA NPs 1:1 (with approx. 84.1% loaded gentamicin) and G-PDA NPs 0.6:1 (with approx. 72.7% loaded gentamicin), were studied. The drug release data were analyzed by LC–MS. The PDA showed good stability in terms of gentamicin release at alkaline pH over a period of seven days. The negative surface charge of PDA at pH 7.4 makes a strong bond with gentamicin, hence preventing its release from the PDA NPs. However, at pH 5 and 3, the amine groups of PDA are more prone towards protonation, making PDA positively charged, hence the repulsive forces caused the gentamicin to detach and release from the G-PDA NPs. Consequently, approx. 40% and 55% drug release were observed at pH 5 and 3, respectively, from the G-PDA NPs 1:1. However, the drug released from G-PDA NPs 0.6:1 was found to be one half as compared to the G-PDA NPs 1:1, which is obvious to the concentration gradient. These findings suggested that the in situ loading method for gentamicin could provide drug release over a period of seven days, hence defending the drug’s efficacy and safety challenges. Furthermore, two kinetic models, namely the Ritger–Peppas and Higuchi models, were implemented to determine the drug release kinetics. Curve fitting analysis supported our findings for the drug release kinetics which are followed by PDA structural changes in response to pH.
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Kumar, B., and G. Jeyabalan. "Development of Anti-diabetic Niosomes Formulation Containing Metformin and Gliclazide." Indian Journal of Pharmaceutical and Biological Research 5, no. 02 (2017): 24–28. http://dx.doi.org/10.30750/ijpbr.5.2.5.
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Metformin/Gliclazide niosomes were formulated with span 60 by ether injection method. Three batches MG1-MG3 were prepared in order to study influence of drug polymer ratio on the niosomes formation and in vitro drug release. The formulated niosomes were characterized by drug entrapment, vesicle size determination, and in vitro drug release. Optimized concentration of span 60 and cholesterol was found to be 1:1. In the in-vitro study, niosomes formulation of MG1 showed high percentage of drug release, 40.18 to 45.75% for about 8 hrs. This indicated that this batch of niosomes formulation exhibit sustained drug release pattern as the niosomes act as reservoir system for continuous delivery of drug. The quantity of Metformin/Gliclazide present in the niosomes and the release medium were estimated by a validated HPLC method. The formulated niosomes had acceptable physicochemical characters and released the drug over 6-8 h. The data obtained from in vitro release studies were fitted with various kinetic models and was found to follow Higuchi kinetics.
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Kotharapu, Rama Koteswararao, and Srinivas Lankalapalli. "Development and Evaluation of Clopidogrel Bisulphate Multi-Unit Floating Mini-Tablets." Journal of Drug Delivery and Therapeutics 9, no. 4 (2019): 173–80. http://dx.doi.org/10.22270/jddt.v9i4.3169.
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The objective of the present work was to formulate and characterize multi-unit floating drug delivery system of Clopidogrel bisulphate to increase the bioavailability and sustain the drug release properties up to 8 h with more predictable drug release kinetics that avoids all or nothing emptying effect wherefore to improve patient compliance. Clopidogrel bisulphate floating mini-tablets were prepared by effervescent approach with melt granulation and direct compression techniques alone and in combination using Hydroxypropyl methylcellulose (HPMC) K100M and Compritol 888 ATO at different concentrations (20%, 30% and 40% w/w) alone and in combination. Sodium bicarbonate at concentration 10% w/w was optimized as gas generating floating agent. Evaluations were carried out on physical parameters, floating behavior and influence of type of polymer on drug release rate of prepared mini tablet formulations. All the formulations were subjected to various quality control and in-vitro dissolution studies and corresponding dissolution data were fitted to popular release kinetic equations in order to evaluate release mechanisms and kinetics. All the Clopidogrel bisulphate floating mini tablet formulations followed zero order kinetics. As per Korsmeyer-Peppas equation, the release exponent “n” ranged 0.561-0.758 indicating that drug release from all the formulations was by non-Fickian diffusion mechanism. Based on the results, Clopidogrel bisulphate floating mini tablets prepared by employing combination of 20% w/w HPMC K100M and 20% w/w Compritol 888 ATO offered desired in-vitro floating time and drug dissolution profile. Keywords: Bioavailability, Clopidogrel bisulphate, floating mini-tablets, release kinetics, sustained release.
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Reddy S, Giridhar. "Kinetic Studies for the Release of Hydroxychloroquine Sulphate Drug (HCQ) In-vitro in Simulated Gastric and Intestinal Medium from Sodium Alginate and Lignosulphonic Acid Blends." Trends in Sciences 20, no. 5 (2023): 5318. http://dx.doi.org/10.48048/tis.2023.5318.
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Biodegradable polymeric blends are used to study the controlled release of Hydroxychloroquine sulphate (HCQ) as the model drug used extensively in COVID-19 treatments. HCQ drug is loaded in sodium alginate (NaAlg) and lignosulphonic acid (NaLS) blends as matrix are crosslinked using calcium chloride solution. Its release is evaluated in different pH mediums of simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). The HCQ release data obtained during experimentation is used to study kinetics using different models to investigate polymeric relaxation's drug diffusion and mechanism in water-soluble HCQ drug. The drug release mechanism best fits the Higuchi model with Fickian diffusion as the primary polymeric relaxation mechanism. HIGHLIGHTS Biodegradable polymer blends of sodium alginate and lignosulphonic acid are loaded with Hydroxychloroquine sulphate to demonstrate and evaluate drug release kinetics in simulated gastric and intestinal gastric fluid Different kinetic models are applied for experimental data to study drug diffusion and polymer relaxation mechanism. Experimental values reveal that pH medium influences drug release The hydroxychloroquine sulphate drug release for extended period in simulated fluids in-vitro proves possible usage for controlled drug delivery applications GRAPHICAL ABSTRACT
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Wang, Lei, and Gang Wu. "Local Delivery System Using Thermosensitive Hydrogel and Drug Loading Microspheres for Cartilage Repairing." Advanced Materials Research 898 (February 2014): 300–303. http://dx.doi.org/10.4028/www.scientific.net/amr.898.300.
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A local drug delivery system constituted by hybrid microsphere/thermosensitive hydrogel was fabricated for Osteoarthritis (OA) therapy in the research. The hydrogel were synthesized by ring-opening copolymerization. Microsphere was fabricated by O/W emulsion and solution evaporation method. The properties of the products were characterized by 1HNMR, FTIR and phase transition diagram. The microsphere/hydrogel was prepared for in vitro drug release research. The results showed microsphere/hydrogel hybrid system can alleviate initial burst release. After 650 hours, only 60 percent of the drugs were released. Kinetics research implied the drug release is controlled by diffusion/erosion mechanism.
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Manalan, B. Valli, Nadendla Swathi, Narra Nandini, et al. "Formulate and evaluate once daily sustained release tablet of highly soluble drug of metformin HCL." International Journal of Research in Pharmaceutical Sciences and Technology 1, no. 4 (2020): 138–45. http://dx.doi.org/10.33974/ijrpst.v1i4.206.
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The aim of the present study was to design an oral sustained release matrix tablet of highly water soluble biguanide anti diabetic drug. The matrix tablets are prepared by melt granulation method using HPMC K 200M as hydrophilic drug release retarding polymer, and stearic acid as melt able binder as well as hydrophobic carrier. The drug and excipients compatibility was studied by FT – IR. The formulated matrix tablets were characterized for physical parameters and in vitro dissolution profile. FT – IR spectra revealed the absence of drug excipients interaction. The physical parameters of the tablets were found within the limits. The drug release kinetics demonstrated that by increasing the concentration of hydrophilic polymer and hydrophobic carrier the drug release rate was retarded proportionally. Kinetic modelling of in vitro release profile revealing that the drug release from the matrix tablets following first order kinetics, and the drug release mechanism of optimized (F7) formula following non fickian transport mechanism. Accelerated stability studies were performed according to ICH guide lines. Temperature 40±20 c and relative humidity 75±5% RH to study physical and chemical changes of formulation. No physical or chemical changes were observed after t accelerated stability studies.
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Haidar, Ziyad S. "Mathematical Modeling for Pharmacokinetic Predictions from Controlled Drug Release Nano Systems: A Comparative Parametric Study." Biomedical and Pharmacology Journal 11, no. 4 (2018): 1801–6. http://dx.doi.org/10.13005/bpj/1552.
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In the present work, several mathematical models well-known in the literature for simulating drug release kinetics are compared using available experimental data sets obtained in real systems with different drugs and nano-sized carriers. Herein, the χ2 minimization method, is employed concluding that the Korsmeyer-Peppas model provides the best-fit in all cases. Hence, (i) better understanding of the exact mass transport mechanism(s) involved in drug(s) release, and (ii) quantitative prediction of the drug release kinetics, can be computed.
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Yin, Wang, Randy Bachelard Nziengui Raby, Yuankai Li, Zuojun Li, Mengqing Sun, and Zhi Huang. "An Alternating Magnetic Field-Controlled Drug Delivery System Based on 4,4′-Azobis (4-Cyanovaleric Acid)-Functioned Fe3O4@Chitosan Nanoparticles." Bioengineering 10, no. 2 (2023): 129. http://dx.doi.org/10.3390/bioengineering10020129.
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Herein, we designed chitosan–coated Fe3O4 nanocomposites for the control release of drugs by an alternating magnetic field (AMF). The chitosan-coated Fe3O4 nanoparticles (Fe3O4@CS) were prepared by a alkaline co-precipitation method, and then, the model drug toluidine blue (TB) was covalently grafted onto the surface of the nanocomposite by a two-step amide reaction with the thermosensitive molecule 4,4′-azobis (4-cyanovaleric acid) (ACVA) as the linker group. The prepared nanocomposites were superparamagnetic and showed high magnetization saturation (about 54.0 emu g-1). In vitro hydrothermal release studies showed that most parts of the TB would be effectively enclosed within the nanocarriers at lower ambient temperatures (23 or 37 °C) due to the molecular bonding of ACVA. The results of kinetic fitting of hydrothermal release data showed that TB released from nanoparticles followed first-order kinetics (R2 > 0.99) and the Korsemeyer–Peppas model (R2 > 0.99, n < 0.5). Most importantly, a single magnetron release experiment demonstrated an approximately linear relationship between the cumulative release of the drug and the duration of action of AMF (R2 = 0.9712). Moreover, the increase in the cumulative release of the drug can be controlled by controlling the switch of the AMF generation device. Therefore, the ACVA-modified Fe3O4@CS nanocarrier designed in this study is a promising model for drug delivery that enables the control of drug release dose by AMF.
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Andreevskaya, SN, TG Smirnova, EN Antonov, et al. "New in vitro model to evaluate kinetics of antimycobacterial drug release from bioresorbable polymeric carriers." MicroRNA in ocular pathology, no. 2020(4) (August 2020): 10–15. http://dx.doi.org/10.24075/brsmu.2020.050.
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Sustained-release drugs against tuberculosis are a promising approach to therapy since they positively affect patient compliance with long regimens, especially when it comes to the multidrug-resistant form of the disease. Conventional UV-visible spectroscopy does not work well with multicomponential culture media used for growing M. tuberculosis. The aim of this study was to develop a method for evaluating the kinetics of anti-tuberculosis drug released from bioresorbable polymeric carriers suitable for screening a wide range of encapsulated prolonged-release drugs and identifying the best performing candidate. While studying the growth dynamics of the laboratory susceptible strain M. tuberculosis H37Rv in the presence of different levofloxacin concentrations (from 0.03 to 0.4 μg/ml), we developed a model, which is essentially a set of 2 parallel experiments evaluating the kinetics of drug release into the culture medium. The results of these 2 experiments conducted on 3 encapsulated forms of levofloxacin loaded onto bioresorbable polymeric PLGA carriers (particles sized 50 μm and 100 μm and the matrix) revealed that release kinetics of the drug largely depended on the type of polymeric carrier. The best encapsulation of the antibiotic and its gradual release into the culture medium was observed for the matrix. All experiments were run in 3 replicates. The obtained data were analyzed using descriptive statistics.
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Joiner, Jordan B., Alka Prasher, Isabella C. Young, et al. "Effects of Drug Physicochemical Properties on In-Situ Forming Implant Polymer Degradation and Drug Release Kinetics." Pharmaceutics 14, no. 6 (2022): 1188. http://dx.doi.org/10.3390/pharmaceutics14061188.
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In-situ forming implants (ISFIs) represent a simple, tunable, and biodegradable polymer-based platform for long-acting drug delivery. However, drugs with different physicochemical properties and physical states in the polymer-solvent system exhibit different drug release kinetics. Although a few limited studies have been performed attempting to elucidate these effects, a large, systematic study has not been performed until now. The purpose of this study was to characterize the in vitro drug release of 12 different small molecule drugs with differing logP and pKa values from ISFIs. Drug release was compared with polymer degradation as measured by lactic acid (LA) release and change in poly(DL-lactide-co-glycolide) (PLGA) molecular weight (MW) measured by size exclusion chromatography with multi-angle laser light scattering (SEC-MALS). Drug physical state and morphology were also measured using differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). Together, these results demonstrated that hydrophilic drugs have higher burst release at 24 h (22.8–68.4%) and complete drug release within 60 days, while hydrophobic drugs have lower burst release at 24 h (1.8–18.9%) and can sustain drug release over 60–285 days. Overall, drug logP and drug physical state in the polymer–solvent system are the most important factors when predicting the drug release rate in an ISFI for small-molecule drugs. Hydrophilic drugs exhibit high initial burst and less sustained release due to their miscibility with the aqueous phase, while hydrophobic drugs have lower initial burst and more sustained release due to their affinity for the hydrophobic PLGA. Additionally, while hydrophilic drugs seem to accelerate the degradation of PLGA, hydrophobic drugs on the other hand seem to slow down the PLGA degradation process compared with placebo ISFIs. Furthermore, drugs that were in a crystalline state within the ISFI drugs exhibited more sustained release compared with amorphous drugs.
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Ghosal, Souvik, Javon E. Walker, and Christopher A. Alabi. "Predictive Platforms of Bond Cleavage and Drug Release Kinetics for Macromolecule–Drug Conjugates." Annual Review of Chemical and Biomolecular Engineering 12, no. 1 (2021): 241–61. http://dx.doi.org/10.1146/annurev-chembioeng-091720-030636.
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Macromolecule–drug conjugates (MDCs) occupy a critical niche in modern pharmaceuticals that deals with the assembly and combination of a macromolecular carrier, a drug cargo, and a linker toward the creation of effective therapeutics. Macromolecular carriers such as synthetic biocompatible polymers and proteins are often exploited for their inherent ability to improve drug circulation, prevent off-target drug cytotoxicity, and widen the therapeutic index of drugs. One of the most significant challenges in MDC design involves tuning their drug release kinetics to achieve high spatiotemporal precision. This level of control requires a thorough qualitative and quantitative understanding of the bond cleavage event. In this review, we highlight specific research findings that emphasize the importance of establishing a precise structure–function relationship for MDCs that can be used to predict their bond cleavage and drug release kinetic parameters.
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Afnan, Muhammad, Hamza Shakeel, Ghulam Mustafa, Waseem Akram, and Talib Husain. "Formulation, development and optimization of ofloxacin FDDS sustained release for UTI and H. pylori." Journal of Contemporary Pharmacy, Vol 8, (1) 2024 (June 30, 2024): 1–8. https://doi.org/10.56770/jcp2024811.
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Objective: Development & Optimization of Ofloxacin Floating tablets to enhance gastric retention time. Sustained release effect of formulation will reduce the dosing frequency for UTIs and prolonged local effect will benefit against H-pylori infection. Materials: Pre formulation tests were performed which include bulk characteristics and flow properties. Post formulation studies include weight variation, thickness, content uniformity, hardness, friability, dissolution studies, release kinetics and compatibility & stability analysis. Kinetic studies were done and models were applied to understand the drug release mechanism. Accelerated stability analysis was also done for time period of 6 months. Results: All pre formulation tests were within range of USP standards, all the formulations showed good buoyancy. The in-vitro dissolution testing showed that F2 released drug at much slower rate, 64.97% within 24 hrs. F3 & F4 released ofloxacin at faster rate, 98.6% & 99.90% respectively, however, F1 released 91.66% drug within 24 hrs. F1 followed Higuchi model, F2 & F3 followed 1st order kinetics and F4 followed 1st order & Higuchi model. For F1, FTIR & DSC analysis curves showed no interaction or change of state of ofloxacin. Conclusion: Formulation F1 was proved to be the optimized formulation and followed non-Fickian release independent of concentration of drug also confirmed from Korsmeyer-Peppas equation. The Stability analysis also proved that F1 is the best fit formulation to be used as Floating Drug Delivery System of Ofloxacin. Stability analysis proved that polymers used in F1 formulation were effective effervescent agents and made the formulation optimized and efficacious.
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Sharma, Megha, Seema Kohli, and Abhisek Pal. "PREPARATION AND EVALUATION OF CONTROLLED RELEASE FLOATING MICROSPHERES OF REPAGLINIDE: OPTIMIZATION AND IN-VITRO STUDIES." Asian Journal of Pharmaceutical and Clinical Research 10, no. 3 (2017): 103. http://dx.doi.org/10.22159/ajpcr.2017.v10i3.15310.
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ABSTRACTObjective: To develop and evaluate floating microspheres of repaglinide (RG).Materials and Methods: RG loaded noneffervescent microspheres of different ratios of ethylcellulose (EC) and hydroxypropyl methylcellulose (HPMCK4M) were prepared using polyvinyl alcohol as emulsifier by solvent evaporation technique. Various process variables such as polymer ratio, stirringspeed, concentration of drug, and emulsifying agent were studied. Compatibility of drug and polymers was studied by Fourier-transform infraredspectroscopy (FTIR). Characterization, in-vitro evaluation, and kinetic studies were performed.Results: FTIR spectra have revealed no drug-excipient incompatibility. The average particle size of microspheres was in the range of 312-359 μm. Theresults showed that floating microspheres were successfully prepared with good yield (56.15-64.3%), high entrapment efficiency (58.22-70.14%),and good floating behavior (63.1-76.2%), respectively. In-vitro release data indicates appreciable amount of drug is released (62.28-73.27%) from themicrospheres in gastric fluid. The mechanism of drug release founds to follow first order kinetics (r2=0.986).Conclusion: The developed floating microspheres of RG may be used for prolonged drug release for at least 12 hrs, thereby improving bioavailabilityand patient compliance.Keywords: Repaglinide, Compatibility, Kinetic, Ethylcellulose.
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Vercik, Luci Cristina de Oliveira, Andres Vercik, and Eliana Cristina da Silva Rigo. "Kinetics of silver nanoparticle release from chitosan spheres." MRS Advances 2, no. 19-20 (2017): 1089–94. http://dx.doi.org/10.1557/adv.2017.48.
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ABSTRACTThe kinetics of silver nanoparticles release from chitosan spheres is addressed experimentally and theoretically in this work. From the experimental viewpoint, the study of silver nanoparticles release is performed by measuring the time-dependent UV-Vis spectra of solutions where spheres were dispersed. The UV-VIS spectra intensity reflects the concentration of nanoparticles in the solution. Despite simple expressions for drug release are found in the literature, as those that relate the amount of drug release with the square root of time, a proper modeling might require the inclusion of several phenomena such as the presence of stagnant layers, swelling or erosion of the matrix, accumulation of particles in the medium, amongst others. The experiments show that chitosan/silver nanoparticles complexes are actually released, indicating that both swelling and erosion of the matrix takes place during the release process. The simplest model for drug release, i.e., the Higuchi’s model, fits the observed results surprisingly well, which is a relevant result due to the lack of mathematical modeling for the release of nanoparticles.
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Suprianto, Suprianto. "ANALISIS KINETIKA PELEPASAN TEOFILIN DARI GRANUL MATRIKS KITOSAN." Jurnal Ilmiah Manuntung 2, no. 1 (2017): 70. http://dx.doi.org/10.51352/jim.v2i1.50.
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Moment the drug dosage form development, it is important to study the drug release or dissolution that is recognized as an element in drug development. Mathematical models could help optimize the design of drugs to produce models of drug release information. Analysis of quantitative values obtained when depicting dissolution drug release profiles more easily when the mathematical concepts used to describe the drug release kinetics model. Model release of drugs known include zero order, first order, Higuchi models, models Hixon Crowell and Peppas Korsmeyer models. The purpose of this review apply mathematical concepts to study the phenomenon of drug release theophylline granules matrix made from chitosan
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Posina Rakshitha, B. Deekshi Gladiola, and Cheepurupalli Prasad. "Formulation and biopharmaceutical evaluation of a transdermal patch containing letrozole." International Journal of Pharmaceuticals and Health Care Research 12, no. 4 (2024): 430–37. https://doi.org/10.61096/ijphr.v12.iss4.2024.430-437.
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The skin can be used as the site for drug administration for continuous transdermal drug infusion into the systemic circulation. For the continuous diffusion penetration of the drugs through the intact skin surface membrane-moderated systems, matrix dispersion type systems, adhesive diffusion controlled systems and micro reservoir systems have been developed. Various penetration enhancers are used for the drug diffusion through skin. In matrix dispersion type systems, the drug is dispersed in the solvent along with the polymers and solvent allowed to evaporate forming a homogeneous drug-polymer matrix. The results obtained showed no physical-chemical incompatibility between the drug and the polymers. L5 formulation has been selected as the best formulation among all the other formulations. The in-vitro drug diffusion studies from the formulation were found to be sustained release. All the evaluation parameters obtained from the best formulation were found to be satisfactory. The data obtained from the in-vitro release studies were fitted to various kinetic models like zero order, first order, Higuchi model and peppas model. From the kinetic data it was found that drug release follows Zero order kinetics model release by diffusion technique from the polymer.
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Radu (Dușman), Ramona-Daniela, and Doina Drăgănescu. "Present and Future of ZrO2 Nanostructure as Reservoir for Drug Loading and Release." Coatings 13, no. 7 (2023): 1273. http://dx.doi.org/10.3390/coatings13071273.
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Extensive research has been conducted on ZrO2 nanostructures due to their favorable biocompatibility, low toxicity, and promising prospects in various biomedical applications. They can be used as drug carriers, facilitating the administration of therapeutic substances into the body while enhancing their effectiveness and safety. This is achieved by regulating the timing, location, and rate at which drugs are released within the body. Several factors can influence the effectiveness of drug loading onto ZrO2 nanostructures, such as the physicochemical characteristics of the drugs, the surface properties of the ZrO2 nanostructures, and the specific methods used for drug loading. A wide range of drugs may be loaded onto ZrO2 nanostructures including anti-cancer drugs, antibiotics, anti-inflammatory drugs, antifungal drugs, anti-osteoporotic drugs, etc. The release kinetics of drugs can be influenced by different factors, such as the size and shape of ZrO2 nanostructures, the pH and temperature of the release medium, and the characteristics and molecular weight of the specific drug being released. While ZrO2 nanostructures have demonstrated significant potential as drug delivery systems, further research on these structures is essential to optimize drug loading and release strategies.
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Krueger, Bailey, Taylor Frazier, Sheila Galbreath, and Tarun Goswami. "Therapeutic efficacies of nano carriers and dissolution kinetics." Journal of Pharmaceutical and Biopharmaceutical Research 4, no. 2 (2022): 296–317. http://dx.doi.org/10.25082/jpbr.2022.02.002.
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The drug dissolution behavior of poorly soluble medication such as doxorubicin has been conducted in this paper. Since the drug was fixed, different carriers used to deliver it and their dissolutions kinetics compiled from literature evaluated in this paper. Even though targeting of drugs is very important in drug delivery, it is not within the scope of this paper. However, functionalization of the carrier may provide this benefit, those constructs are included for comparison in terms of hybrid constructs. Dendrimer, micelles and hybrid constructs used in the delivery of doxorubicin compared in this paper with respect to carrier size and drug loading. Assuming that the dissolution follows a slow release, 40-50% of the drug in the phase I representing the sudden or the burst release, followed by a steady release of 50-60% of the drug in phase II, not all the carriers and their sizes exhibited this behavior. Carriers and hybrid constructs 38nm size were more effective where phase I and II was observed, however, as the size decreased to 34 nm or increased, dissolution kinetics with minimal release occurred meaning the carriers were too big to penetrate the vasculature permeability. Nano-carriers, dendrimers, micelle, hybrid dendrimers, and hybrid micelle were found to be effective with the carrier manufacturing, generation, polymer, molecular weight of the carrier and other parameters. The release rate of doxorubicin was found to be effective with dendrimers together with hybrid dendrimer exhibiting a bilinear kinetics. Micelles 20nm were more effective representing 60% of release in 10 hours followed by additional 25% in 35 hours exhibiting a bilinear behavior. Size greater than 20nm resulted in slow dissolution reaching less than 10 to 40% of drug. Several drugs exhibited multiple slopes in their dissolution kinetics when micelle was used. The therapeutic efficacy of hybrid micelle was superior to other nano-carriers.
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Ebadi, Mona, Kalaivani Buskaran, Bullo Saifullah, Sharida Fakurazi, and Mohd Zobir Hussein. "The Impact of Magnesium–Aluminum-Layered Double Hydroxide-Based Polyvinyl Alcohol Coated on Magnetite on the Preparation of Core-Shell Nanoparticles as a Drug Delivery Agent." International Journal of Molecular Sciences 20, no. 15 (2019): 3764. http://dx.doi.org/10.3390/ijms20153764.
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One of the current developments in drug research is the controlled release formulation of drugs, which can be released in a controlled manner at a specific target in the body. Due to the diverse physical and chemical properties of various drugs, a smart drug delivery system is highly sought after. The present study aimed to develop a novel drug delivery system using magnetite nanoparticles as the core and coated with polyvinyl alcohol (PVA), a drug 5-fluorouracil (5FU) and Mg–Al-layered double hydroxide (MLDH) for the formation of FPVA-FU-MLDH nanoparticles. The existence of the coated nanoparticles was supported by various physico-chemical analyses. In addition, the drug content, kinetics, and mechanism of drug release also were studied. 5-fluorouracil (5FU) was found to be released in a controlled manner from the nanoparticles at pH = 4.8 (representing the cancerous cellular environment) and pH = 7.4 (representing the blood environment), governed by pseudo-second-order kinetics. The cytotoxicity study revealed that the anticancer delivery system of FPVA-FU-MLDH nanoparticles showed much better anticancer activity than the free drug, 5FU, against liver cancer and HepG2 cells, and at the same time, it was found to be less toxic to the normal fibroblast 3T3 cells.
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Parashar, Tarun, Kapil Kalra, Jyoti M. Kalra, et al. "Formulation and In-vitro Evaluation of Bilayer Tablet of Olmesartan Medoxomil for Biphasic Drug Release." INTERNATIONAL JOURNAL OF PHARMACEUTICAL QUALITY ASSURANCE 14, no. 02 (2023): 388–92. http://dx.doi.org/10.25258/ijpqa.14.2.24.
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Objective: The current study aimed to optimize the bioavailability and absorption of olmesartan in the lower gastrointestinal tract by creating a bilayer tablet for biphasic drug release. Methods: Microcrystalline cellulose was combined and direct compression the requirement for an early response to address an undesirable defect or condition. In the current instance, 5 mg of olmesartan must be released immediately, and the remaining 10 mg of olmesartan must be released gradually to maintain the therapeutic concentration. In order to adjust the release pattern of the olmesartan sustained release tablet in accordance with the needs of therapy and IP guidelines. Result: The best cumulative drug release was demonstrated by formulation. All formulations for immediate release support the first-order kinetics. As a result, all three formulations were chosen for additional research. Dissolution rate for long-term release Cumulative drug release from the SR1 to SR3 formulations using HPMC K15M and gum acacia was up to 24 hours. Utilizing HPMC K15M and guar gum, the formulations SR1, SR2, and SR3 demonstrated cumulative drug releases of 72.66, 69.19, and 92.66%, respectively. The best cumulative release of the drug was demonstrated by formulations SR1, SR2, and SR3. Consequently, everyone was chosen for additional research. The cumulative drug release for the IR1-SR1, IR2-SR2, and IR3-SR3 bilayer tablet formulations was 95.24, 90.15, and 91.09%. Up to 12 hours of cumulative drug release from the formulation was observed. As a result, it was determined that IR1-SR1 was the best formulation out of all of them due to its strong correlation between the total cumulative percentage of medication releases and time, which was 95.24% up to 12 hours.
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Chandra, Prakash Sunuwar* Meenakshi Kandwal Shivanand Patil. "A Review on Formulation and Evaluation of Mirabegron Extended-Release Tablets." International Journal of Pharmaceutical Sciences 3, no. 5 (2025): 4859–65. https://doi.org/10.5281/zenodo.15547921.
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A type of modified-release dosage form known as an extended-release (ER) tablet is designed to release the active pharmaceutical ingredient (API) gradually over a long period of time. The human body metabolizes and excretes drugs at different rates. Fast drug absorption may result in peak plasma concentrations that could be harmful, whereas fast clearance in conventional formulations causes subtherapeutic levels that necessitate frequent dose. Extended-release formulations get around these issues and ensure a long-lasting therapeutic effect by modifying the kinetics of medicine release. This study includes Extended-Release Tablets' Drug Release Mechanism, benefits of extended-release tablet, limitations, Extended-release tablet development and manufacturing.
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Damiri, Fouad, Yahya Bachra, Chaimaa Bounacir, Asmae Laaraibi, and Mohammed Berrada. "Synthesis and Characterization of Lyophilized Chitosan-Based Hydrogels Cross-Linked with Benzaldehyde for Controlled Drug Release." Journal of Chemistry 2020 (May 18, 2020): 1–10. http://dx.doi.org/10.1155/2020/8747639.
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In this study, chitosan-based hydrogels were produced by incorporating three drugs with a different solubility into a polymer matrix. The lyophilized chitosan salt was prepared using an innovative and less-expensive synthetic process by the freeze-drying technique. Firstly, the three drugs (caffeine, ascorbic acid, and 5-fluorouracil (5-FU)) were selected as model drugs to test the in vitro release behavior of the hydrogel. The drugs were solubilized in chitosan salt, lyophilized, and cross-linked with benzaldehyde involving the formation of a Schiff base with (–C=N-) linkage to produce a physical hydrogel. Subsequently, the physicochemical properties of N-benzyl chitosan and lyophilized chitosan salt were evaluated by Fourier-transform infrared (FTIR) spectra, scanning electron microscopy (SEM), and thermogravimetric analysis (TGA). The intrinsic viscosity of the conventional chitosan was determined by the Mark–Houwink–Sakurada equation. Moreover, the kinetics of hydrogel swelling and drug release were studied by the UV-visible method at physiological conditions (pH = 7.4 at 37°C). The results show that lyophilized N-benzyl chitosan had a maximum swelling ratio of 720 ± 2% by immersion in phosphate-buffered saline solutions (PBS) (pH = 7.4 at 37°C). In vitro drug releases were evaluated in PBS, and the obtained results show that the maximum drug release after 24 h was 42% for caffeine, 99% for 5-FU, and 94% for ascorbic acid. Then, to optimize the cumulative release of caffeine, Tween 20 was added and 98% as a release percentage was obtained. The drug-loading results were investigated with the Korsmeyer–Peppas kinetic model and applied to determine the drug release mechanism.
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Kundrat, Vojtech, Nicole Cernekova, Adriana Kovalcik, Vojtech Enev, and Ivana Marova. "Drug Release Kinetics of Electrospun PHB Meshes." Materials 12, no. 12 (2019): 1924. http://dx.doi.org/10.3390/ma12121924.
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Microbial poly(3-hydroxybutyrate) (PHB) has several advantages including its biocompatibility and ability to degrade in vivo and in vitro without toxic substances. This paper investigates the feasibility of electrospun PHB meshes serving as drug delivery systems. The morphology of the electrospun samples was modified by varying the concentration of PHB in solution and the solvent composition. Scanning electron microscopy of the electrospun PHB scaffolds revealed the formation of different morphologies including porous, filamentous/beaded and fiber structures. Levofloxacin was used as the model drug for incorporation into PHB electrospun meshes. The entrapment efficiency was found to be dependent on the viscosity of the PHB solution used for electrospinning and ranged from 14.4–81.8%. The incorporation of levofloxacin in electrospun meshes was confirmed by Fourier-transform infrared spectroscopy and UV-VIS spectroscopy. The effect of the morphology of the electrospun meshes on the levofloxacin release profile was screened in vitro in phosphate-buffered saline solution. Depending upon the morphology, the electrospun meshes released about 14–20% of levofloxacin during the first 24 h. The percentage of drug released after 13 days increased up to 32.4% and was similar for all tested morphologies. The antimicrobial efficiency of all tested samples independent of the morphology, was confirmed by agar diffusion testing.
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G.Jagadeesh*, Dr.Vijaya Kuchana. "DESIGN AND INVITRO CHARACTERIZATION OF GASRO RETENTIVE MUCOADHESIVE FLOATING TABLETS OF METFORMIN HCL." Indo American Journal of Pharmaceutical Sciences 04, no. 09 (2017): 3202–9. https://doi.org/10.5281/zenodo.936410.
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In the present research work gastro retentive mucoadhesive floating formulation of Metformin was developed by using various hydrophilic polymers. Initially analytical method development was done for the drug molecule. Absorption maxima was determined based on that calibration curve was developed by using different concentrations. Gas generating agent accrual and bioadhesive polymer carbopol concentration was optimized. Then the formulation was developed by using different concentrations of polymers of various polymers. The formulation blend was subjected to various preformualation studies, flow properties and all the formulations were found to be good indicating that the powder blend has good flow properties. Among all the formulations the formulations prepared with HPMC K15M retarded the drug release up to 12 hours in the concentration of 220mg (F10).The formulations prepared with HPMC K4M and HPMC K100M released drug less than 12 hours. Hence they were not considered. The optimized formulation dissolution data was subjected to release kinetics, from the release kinetics data it was evident that the formulation followed zero order kinetics of drug release. Key words: Gastro retentive, Mucoadhesive, Floating, HPMC etc.
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Ashok, Kumar. S., S. Duraivel., and Pragathikumar.B. "Design, Development and Evaluation of Bilayered Tablets Containing Amlodipine Besilate as Immediate Release and Metprolol Succinate as Sustained Release." International Journal of Current Pharmaceutical Review and Research 3, no. 4 (2013): 130–43. https://doi.org/10.5281/zenodo.12691440.
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Bilayer tablets of Amlodipine besilate (IR) Metoprolol succinate (SR) were formulated for the management ofhypertension. In the formulation of immediate release sodium starch glycolate were used as super disintegrantand was directly compressed. For sustained release portion HPMC polymers were used in granulationstage . Preformulation studies were performed prior to compression. The compressed bilayer tablets wereevaluated for weight variation, dimension, hardness, friability, drug content, disintegration time and invitrodrug release using USP dissolution apparatus type 2 (paddle). It was found that the optimized formulationshowed 15.98%, 39.04%, 58.76%, 94.86%release for Metoprolol succinate in 1, 4, 8, 20 hoursrespectively.However, Amlodipine besilatereleased 95% at the end of 45 minutes.The IR spectrum and DSCstudies revealed that there is no disturbance in the principal peaks of pure drugs Metoprolol succinate andAmlodipinebesilate. This further confirms the integrity of pure drugs and no incompatibility of them withexcipients. The stability studies were carried out for the optimized batch for three months and it showedacceptable results. The kinetic studies of the formulations revealed that diffusion is the predominant mechanismof drug and release follows first order kinetics.
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Iovanov, Rareș Iuliu, Ioan Tomuță, and Sorin Emilian Leucuța. "Development of a reservoir type prolonged release system with felodipine via simplex methodology." Medicine and Pharmacy Reports 89, no. 1 (2015): 128–36. http://dx.doi.org/10.15386/cjmed-526.
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Background and aims. Felodipine is a dihydropyridine calcium antagonist that presents good characteristics to be formulated as prolonged release preparations. The aim of the study was the formulation and in vitro characterization of a reservoir type prolonged release system with felodipine, over a 12 hours period using the Simplex method.Methods. The first step of the Simplex method was to study the influence of the granules coating method on the felodipine release. Furthermore the influence of the coating polymer type, the percent of the coating polymer and the percent of pore forming agent in the coating on the felodipine release were studied. Afterwards these two steps of the experimental design the percent of Surelease applied on the felodipine loaded granules and the percent of pore former in the polymeric coating formulation variables were studied. The in vitro dissolution of model drug was performed in phosphate buffer solution (pH 6.5) with 1% sodium lauryl sulfate. The released drug quantification was done using an HPLC method. The release kinetics of felodipine from the final granules was assessed using different mathematical models.Results. A 12 hours release was achieved using granules with the size between 315 – 500 µm coated with 45% Surelease with different pore former ratios in the coating via the top-spray method.Conclusion. We have prepared prolonged release coated granules with felodipine using a fluid bed system based on the Simplex method. The API from the studied final formulations was released over a 12 hours period and the release kinetics of the model drug substance from the optimized preparations fitted best the Higuchi and Peppas kinetic models.